Phenanthroindolizidine and phenanthroquinolizidine derivatives constitute a series of compounds that
are being intensively studied as potential anticancer agents. Related natural products such as antofine and
tylophorine alkaloids are well known for their high cytotoxic activity; however, their clinical application has been
limited because of their side effects. In this review we report, in detail, on the main structural modifications
applied to the phenanthroindolizidine and phenanthroquinolizidine skeletons, and we also describe their associated
anticancer activities. New derivatives with promising antitumoral activities have emerged. Simplified analogues were prepared using
rapid synthetic routes, and a certain number of these analogues displayed increased anticancer activity and selectivity towards tumor cell
lines. It is hoped that a better understanding of the mechanisms of action associated with structure–activity relationships (SAR) will
enable us to rationalize the development of new anticancer drugs.
Keywords: Alkaloids, anticancer, antofine, phenanthroindolizidine, phenanthroquinolizidine, structure–activity relationships, tylophorine.
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